Tissue cholinesterase inhibition by propranolol and related drugs

Alkondon, M.; Ray, A.; Sen, P.

Journal of Pharmacy and Pharmacology 38(11): 848-850

1986


ISSN/ISBN: 0022-3573
PMID: 2879019
Document Number: 274242
The effect of (.+-.)-propranolol and some related drugs have been investigated on the cholinesterase (ChE) enzyme activity of heart and brain tissues of the rat. Brain homogenates hydrolysed more methacholine than benzoylcholine and the reverse was true for the heart tissue. In-vitro, (.+-.)-, (+)- and (-)-propranolol, as well as it's quaternary analogue, UM-272, all significantly inhibited heart and brain ChE. Timolol and scotalol, however, were less potent. In-vitro, (.+-.)-propranolol (30 .mu.mol kg-1) significantly inhibited brain ChE activity in rats when compared with saline controls. It is inferred that propranolol inhibits brain and heart ChE enzyme in a non-stereoselective manner and that this cholinomimetic action could be involved in the mediation of some of it's therapeutic effects.

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